An inhibitor of both FLT3 and JAK2 (IC50s = 22 and 23 nM

Pacritinib – 500 µg

Brand:
Cayman
CAS:
937272-79-2
Storage:
-20
UN-No:
Non-Hazardous - /

FMS-like tyrosine kinase 3 (FLT3) and Janus kinase 2 (JAK2) are tyrosine kinases that mediate cytokine signaling and are frequently mutated in cancers, particularly acute myeloid leukemia.{27422,27424} Pacritinib is an inhibitor of both FLT3 and JAK2 (IC50s = 22 and 23 nM, respectively).{27422} It also blocks the activities of the FLT3 D835Y mutant, FLT3 with internal tandem duplications (ITDs), and JAK2 with a V617F substitution (IC50s = 6, 20-180, and 220 nM, respectively).{27422} Pacritinib also inhibits JAK1, JAK3, and TYK2 (IC50s = 1280, 520, and 50 nM, respectively).{27422} Pacritinib is orally bioavailable, inhibiting FLT3 and JAK2 signaling, tumor growth, and metastasis in xenografts in mice.{27422} It is synergistic with the histone deacetylase inhibitor pracinostat (also known as SB 939, Item No. 10443), decreasing cell proliferation and inducing apoptosis in cells carrying either the JAK2 V617F mutation or FLT3 with ITDs, both in vitro and in vivo.{27423} Pacritinib has potential in resolving hematological malignancies.{27424}  

 

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Description

An inhibitor of both FLT3 and JAK2 (IC50s = 22 and 23 nM, respectively); blocks the activities of the FLT3 D835Y mutant, FLT3 with ITDs, and JAK2 with a V617F substitution (IC50s = 6, 20-180, and 220 nM, respectively); orally bioavailable, inhibiting tumor growth and metastasis in xenografts in mice

Formal name: 11-[2-(1-pyrrolidinyl)ethoxy]-14,19-dioxa-5,7,27-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16E,21,23-decaene

Synonyms:  SB1518

Molecular weight: 472.6

CAS: 937272-79-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JAK Family||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cell Biology|Cell Signaling|JAK Signaling

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